Etifoxine
Encyclopedia
Etifoxine is an anxiolytic
and anticonvulsant
drug developed by Hoechst in the 1960s. It is used in anxiety disorders and to promote peripheral nerve healing. It has similar effects to benzodiazepine
drugs, but is structurally distinct and does not bind to the benzodiazepine receptor. It is more effective than lorazepam
as an anxiolytic, and has fewer side effects.
Etifoxine has been associated with acute liver injury.
receptor
complex, and so is acting at a different target site to benzodiazepines, although the physiological effect that is produced is similar to that of benzodiazepines. This difference in binding means that etifoxine can be used alongside benzodiazepines to potentiate their effects without competing for binding sites, however it also means that the effects of etifoxine are not reversed by the benzodiazepine antagonist flumazenil
.
Anxiolytic
An anxiolytic is a drug used for the treatment of anxiety, and its related psychological and physical symptoms...
and anticonvulsant
Anticonvulsant
The anticonvulsants are a diverse group of pharmaceuticals used in the treatment of epileptic seizures. Anticonvulsants are also increasingly being used in the treatment of bipolar disorder, since many seem to act as mood stabilizers, and in the treatment of neuropathic pain. The goal of an...
drug developed by Hoechst in the 1960s. It is used in anxiety disorders and to promote peripheral nerve healing. It has similar effects to benzodiazepine
Benzodiazepine
A benzodiazepine is a psychoactive drug whose core chemical structure is the fusion of a benzene ring and a diazepine ring...
drugs, but is structurally distinct and does not bind to the benzodiazepine receptor. It is more effective than lorazepam
Lorazepam
Lorazepam is a high-potency short-to-intermediate-acting 3-hydroxy benzodiazepine drug that has all five intrinsic benzodiazepine effects: anxiolytic, amnesic, sedative/hypnotic, anticonvulsant, antiemetic and muscle relaxant...
as an anxiolytic, and has fewer side effects.
Etifoxine has been associated with acute liver injury.
Mechanism of action
Unlike benzodiazepines, etifoxine appears to produce its anxiolytic effects by binding to β2 and β3 subunits of the GABAAGABA A receptor
The GABAA receptor is an ionotropic receptor and ligand-gated ion channel. Its endogenous ligand is γ-aminobutyric acid , the major inhibitory neurotransmitter in the central nervous system. Upon activation, the GABAA receptor selectively conducts Cl- through its pore, resulting in...
receptor
Receptor (biochemistry)
In biochemistry, a receptor is a molecule found on the surface of a cell, which receives specific chemical signals from neighbouring cells or the wider environment within an organism...
complex, and so is acting at a different target site to benzodiazepines, although the physiological effect that is produced is similar to that of benzodiazepines. This difference in binding means that etifoxine can be used alongside benzodiazepines to potentiate their effects without competing for binding sites, however it also means that the effects of etifoxine are not reversed by the benzodiazepine antagonist flumazenil
Flumazenil
Flumazenil is a benzodiazepine antagonist available for injection only, and the only benzodiazepine receptor antagonist on the market today.It was first introduced in 1987 by Hoffmann-La Roche under the trade name Anexate, but only approved by...
.